2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Vilanterol acetate

Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

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CAS No. : 503068-35-7

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Vilanterol acetate Related Antibodies

Top Publications Citing Use of Products

    Vilanterol acetate purchased from MedChemExpress. Usage Cited in: University of Alberta. 2016 Sep.

    The objective of the next set of experiments is to determine if the (i) super long-acting 2-AR agonists Indacaterol and Vilanterol inhibit TNF-α in a β-arrestin2-dependent manner, and (ii) whether β-arrestin2 is involved in the anti-inflammatory conversion leading to the up-regulation of IL-10 production by these β2-AR agonists.

    Vilanterol acetate purchased from MedChemExpress. Usage Cited in: University of Alberta. 2016.

    β-arrestin2 is important in the β2-AR agonist-mediated inhibition of TNF-β, but not in β2-AR agonist-mediated IL-10 enhancement. Western blot showing silencing β-arrestin2 expression.

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    Description

    Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

    In Vitro

    Vilanterol acetate (Compound 13f) is a highly efficient (β2: pEC50 = 9.4), highly active (IA = 0.69), and highly selective (pEC50 difference: β2/β1 = 3.0) β₂ receptor agonist in CHO cells transfected with human β1, β2, and β3 receptors[1].

    Vilanterol acetate (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments[1].

    Vilanterol acetate has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption[1].

    Vilanterol acetate is highly selective for β2-AR, with at least 1000-fold selectivity for the β2-AR and β3-AR subtypes[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Vilanterol acetate Related Antibodies
    Parmacokinetics
    Species Dose Route CLplasma Cmax
    Rat 0.25 mg/kg i.v. 123 mL/min/kg /
    Rat 2 mg/kg p.o. / <2 ng/mL
    In Vivo

    Vilanterol acetate (Compound 13f) (30 μM, 300 μM, Nebulizer inhalation, Once dose) exerts a long-lasting effect on in vivo bronchial dilation following inhalation. The higher the administered dose, the longer the duration of this effect, and it can significantly alleviate asthma symptoms in histamine-induced bronchospasm in the guinea pig[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Histamine-induced bronchospasm in the guinea pig model[1]
    Dosage: EC90 = 30 μM, 300 μM
    Administration: Nebulizer inhalation (Neb. Inh.), once dose.
    Result: Exhibited a duration of action of 10 hours at an EC90 of 30 μM and 17 hours at an EC90 of 300 μM.
    Molecular Weight

    546.48

    Formula

    C26H37Cl2NO7
    CAS No.
    SMILES

    OC1=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO.CC(O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    Vilanterol acetate Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vilanterol503068-35-7GW642444GW 642444GW-642444Adrenergic ReceptorBeta ReceptorCHO cellsMDCKII-MDR1 cellsguinea pigAsthmaChronic Obstructive Pulmonary Disease (COPD)Inhibitorinhibitorinhibit

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